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Assay Detail

CHEMBL903519

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Functional
Antiproliferative activity against human N87 cells
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-N87
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-N87 (CHEMBL614197)
Type CELL-LINE
Organism Homo sapiens

Publication

New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Mastalerz H, Chang M, Chen P, Dextraze P, Fink BE, Gavai A, Goyal B, Han WC, Johnson W, Langley D, Lee FY, Marathe P, Mathur A, Oppenheimer S, Ruediger E, Tarrant J, Tokarski JS, Vite GD, Vyas DM, Wong H, Wong TW, Zhang H, Zhang G.
Bioorg Med Chem Lett (2007) 17 : 2036 -2042
PubMed 17270437 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.11 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL246284 1 7.08
CHEMBL428046 1 6.89
CHEMBL245278 1 6.89
CHEMBL396079 1 6.62
CHEMBL245869 1 6.48
CHEMBL427671 1 6.42
CHEMBL247127 1 6.26
CHEMBL246493 1 6.21
CHEMBL245667 1 6.19
CHEMBL394495 1 6.18
CHEMBL246072 1 6.14
CHEMBL246073 1 6.01
CHEMBL246694 1 5.77
CHEMBL246491 1 5.77
CHEMBL394333 1 5.77
CHEMBL395591 1 5.70
CHEMBL245277 1 5.66
CHEMBL246492 1 5.52
CHEMBL395883 1 5.47
CHEMBL246276 1 5.13
CHEMBL394056 1 -
CHEMBL246489 1 -
CHEMBL397122 1 -
CHEMBL394057 1 -
CHEMBL245867 1 -
CHEMBL245868 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL246284 IC50 = 83.0 nM 7.08
CHEMBL428046 IC50 = 130.0 nM 6.89
CHEMBL245278 IC50 = 130.0 nM 6.89
CHEMBL396079 IC50 = 240.0 nM 6.62
CHEMBL245869 IC50 = 330.0 nM 6.48
CHEMBL427671 IC50 = 380.0 nM 6.42
CHEMBL247127 IC50 = 550.0 nM 6.26
CHEMBL246493 IC50 = 610.0 nM 6.21
CHEMBL245667 IC50 = 640.0 nM 6.19
CHEMBL394495 IC50 = 660.0 nM 6.18
CHEMBL246072 IC50 = 720.0 nM 6.14
CHEMBL246073 IC50 = 980.0 nM 6.01
CHEMBL246694 IC50 = 1700.0 nM 5.77
CHEMBL246491 IC50 = 1700.0 nM 5.77
CHEMBL394333 IC50 = 1700.0 nM 5.77
CHEMBL395591 IC50 = 2000.0 nM 5.70
CHEMBL245277 IC50 = 2200.0 nM 5.66
CHEMBL246492 IC50 = 3000.0 nM 5.52
CHEMBL395883 IC50 = 3400.0 nM 5.47
CHEMBL246276 IC50 = 7400.0 nM 5.13
CHEMBL394056 IC50 - -
CHEMBL246489 IC50 - -
CHEMBL397122 IC50 - -
CHEMBL394057 IC50 > 10000.0 nM -
CHEMBL245867 IC50 - -
CHEMBL245868 IC50 - -